CHOLINOMIMETI

CS

Neurotransmitter

Acetylcholine
Parasympathe Receptors

tic

system

Muscarinic
Nicotinic

Acetylcholi
ne

Muscarinic

Recept
ors
Nicotinic

Cholinomimetics are drugs

that mimic action of
acetylcholine (Ach) at its
receptors
Directly
Indirectly

DIRECTYLY ACTING
CHOLINOMIMETICS

Choline
esters

CLASSIFICATI
ON

Cholinomime
tic
alkaloids

Acetylcholine
Methacholine

Mainly
Muscarinic
Agonists

Carbachol
Bethanechol

Mainly
Nicotinic
Agonists

Mainly Muscarinic
Agonists
Natural Alkaloids
CLASSIFICATI
ON

Muscarine
Pilocarpine
Arecholine

Synthetic Alkaloids
Oxotremorine
Aceclidine
Cervimiline

Mainly Nicotinic Agonoists

Natural Alkaloids
CLASSIFICATI
ON

Nicotine
Lobeline

Synthetic Alkaloids
Dimethylphenylpiperazinium(DM
PP)

PH
IC AR
S
M
AC
OK
IN
T

Choline
esters

Quarternary amines
Resistant to hydrolysis by
esterase

Choline
alkaloids

Tertiary amines

MUSCARINIC
ACTIONS

EYE
M3 receptors
pupillary constrictor muscle
ciliary muscle
lacrimal gland

M3

Ciliary body
M3

Pupillary
constrictor
M3

M3

LUNGS
Bronchoconstriction
tracheobronchial secretions

GASTROINTESTINAL TRACT
M3 receptor
amplitude of contractions
relax sphincter
secretions

URINARY TRACT
M3 receptors
contraction of detrusor
relaxation of sphincter

SA node
AV node
Atria >
ventricles

HEART

M2 (heart), M3 (blood vessels)

heart rate

conduction through AV node

force of contraction

vasodilation

CNS
Brain is rich in M & SC in N receptors
Activation of M1 --- slow excitation of neuron
Important role in cognitive function specially memory (M1)

Pre-senile dementia of Alzheimer type ----loss of cholinergic

neurons.

NICOTINIC
ACTIONS

 Autonomic ganglia , Adrenal

medulla
N.M .Junction
Central Nervous System

 Ophthalmology

THERAPEUTI
C
APPLICATIO
NS
(MUSCARINIC)

Xerostomia

(Pilocarpine)

Miotic agent
Glaucoma

(Pilocarpine ,cevimeline)

Sjorgens syndrome (Pilocarpine)

Increase gastrointestinal motility
(Bethanechol)

Urinary retention
(Bethanechol)

Diagnosis of bronchial airway reactivity

(Methacholine)

 Direct-acting nicotinic agonists have

no therapeutic applications except in
THERAPEUTI smoking cessation
C
Varenicline is a newer nicotinic
APPLICATIO
agonist
with
partial
agonist
NS
properties.
It
appears
to
reduce
(NICOTINIC)
craving in persons addicted to
nicotine

Cramps and diarrhea

Urination (Detrusor contraction and Sphincter

relaxation)
Urinary frequency

Muscle (Skeletal) excitation

Twitchings and fasciculations

ADVERS
E
EFFECT
S

Bronchospasm
Shortness of breathe (Dyspnea)

Heart bradycardia and reduced contractility,

conductivity
Bradycardia

Autonomic ganglia stimulation

Vascular dilation (hypotenstion)
Hypotension

Eye miosis and accomodation spasm

Blurred vision

Secretions increase (lacrimation, sweating, salivation,

GI secretions)
increased sweating and salivation

Stimulation followed by depression in CNS

 Signs of muscarinic excesssalivation, sweating, nausea,

MUSHROO
M
POISONIN
G

vomiting,diarrhea,visual
disturbances, headache, abd. colic,
urinary urgency, bradycardia,
bronchospasm, hypotension, shock
Atropine (1-2mg I/M every 30mins)

A. CNS stimulation, cause

convulsions, coma and
respiratory arrest.

ACUTE
NICOTINE
TOXICITY

B. Skeletal muscle depolarization

and respiratory paralysis.
C. Hypertension and cardiac
arrhythmia

 Bronchial asthma
Recent myocardial infarction
CONTRAINDICATIO
NS

Coronary insufficiency
GI or urinary tract obstruction
Peptic ulcer
Hyperthyroidism